- OXAZOLE TYROSINE KINASE INHIBITORS
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The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1 : provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.
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Page/Page column 96
(2009/01/20)
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- TRIAZOLOANILINOPYRIMIDINE DERIVATIVES FOR USE AS ANTIVIRAL AGENTS
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A quinazoline derivative of formula (I), or a pharmaceutically acceptable salt thereof: formula (I) for use in treatment of prevention of a flaviviridae infection.
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Page/Page column 42
(2010/11/28)
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- Regio- and stereoselective route to tetrasubstituted olefins by the palladium-catalyzed three-component coupling of aryl iodides, internal alkynes, and arylboronic acids
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The Pd-catalyzed three-component coupling of readily available aryl iodides, internal alkynes, and arylboronic acids provides a convenient, one-step, regio- and stereoselective route to tetrasubstituted olefins in good to excellent yields, although electron-poor aryl iodides and dialkylalkynes normally afford only low yields under our standard reaction conditions. The proper combination of substrates and reaction conditions is important for high yields. The presence of water generally substantially increases the yields of the desired tetrasubstituted olefins. The reaction involves cis-addition of the aryl group from the aryl iodide to the less hindered or more electron-rich end of the alkyne, while the aryl group from the arylboronic acid adds to the other end. A modified, room-temperature procedure has also been successfully developed, which works very well for some substrates. Tamoxifen and its derivatives are synthesized in a concise, regio- and stereoselective manner by applying our synthetic protocol.
- Zhou, Chengxiang,Larock, Richard C.
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p. 3765 - 3777
(2007/10/03)
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- Biphenyl compounds and their use as oestrogenic agents
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Compounds of formula (I), wherein [X] represents aromatic carbocyclic rings (A) and (B), where R1, R2, R3, R4, R5, R6and R7are as defined in the description, salts thereof, a method and intermediates for preparing same, the use thereof as drugs, and pharmaceutical compositions containing same, are disclosed.
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Page column 9-10
(2010/11/29)
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